ChemicalBook > Product Catalog >Biochemical Engineering >Inhibitors >Epigenetics >Epigenetic Reader Domain inhibitors >RVX-208

RVX-208

RVX-208 Structure
CAS No.
1044870-39-4
Chemical Name:
RVX-208
Synonyms
CS-686;CS-1815;RVX-208;RVX-000222;Apabetalone;RVX-208 USP/EP/BP;RVX-208(RVX000222);RVX-208(RVX 000222);Apabetalone-RVX-208;Apabetalone (RVX-08, RVX-000222)
CBNumber:
CB52640278
Molecular Formula:
C20H22N2O5
Molecular Weight:
370.4
MOL File:
1044870-39-4.mol
MSDS File:
SDS
Modify Date:
2023/9/4 15:50:00

RVX-208 Properties

Boiling point 594.2±60.0 °C(Predicted)
Density 1.28±0.1 g/cm3(Predicted)
storage temp. -20°C (des.)
solubility Soluble in DMSO (up to 75 mg/ml) or in Ethanol (up to 4 mg/ml).
form solid
pka 14.21±0.10(Predicted)
color White
Stability Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 1 month.

SAFETY

Risk and Safety Statements

Symbol(GHS) 
GHS08
Signal word  Warning
Hazard statements  H371
Precautionary statements  P260-P264-P270-P309+P311-P405-P501

RVX-208 Chemical Properties,Uses,Production

Description

The bromodomain and extra terminal (BET) proteins interact with acetylated lysine-containing sequences on target proteins via their bromodomains, commonly altering gene transcription. The human BET proteins contain two bromodomains, the first (BD1) being closer to the N-terminus than the second (BD2). RVX-208 is a selective antagonist of BET bromodomains, binding with 10-100-fold higher affinity for BD2 (IC50 = 0.04-0.28 μM) over BD1 (IC50 = 1.8-3.1 μM). RVX-208 causes the selective release of BET proteins from chromatin in cells. It interferes with the BET protein BRD4, resulting in an increased expression of apolipoprotein (Apo) A1 in cells, mice, monkeys, and humans. RVX-208 also reduces atherosclerosis in hyperlipidemic ApoE-deficient mice.

Uses

RVX-208 is a selective antagonist of bromodomain and extra terminal (BET)’s bromodomains.

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2-(4-(2-hydroxyethoxy)-3,5-diMethylphenyl)-5,7-diMethoxyquinazolin-4(3H)-one RVX-000222 4(3H)-Quinazolinone, 2-[4-(2-hydroxyethoxy)-3,5-dimethylphenyl]-5,7-dimethoxy- 2-[4-(2-hydroxyethoxy)-3,5-dimethylphenyl]-5,7-dimethoxy-4(3H)-quinazolinone RVX-208 RVX-208 Apabetalone Apabetalone-RVX-208 RVX-208(RVX 000222) RVX-208(RVX000222) CS-1815 APABETALONE; RVX-000222; RVX208; RVX 208; RVX000222; RVX 000222 CS-686 RVX-208 USP/EP/BP Apabetalone (RVX-08, RVX-000222) Apabetalone (RVX-208, RVX-000222) 2-(4-(2-Hydroxyethoxy)-2,6-dimethylphenyl)-6,8-dimethoxyquinazolin-4(3H)-one 1044870-39-4 Inhibitors API